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    Allosteric modulators of the A1 adenosine receptor
    1.
    发明授权
    Allosteric modulators of the A1 adenosine receptor 失效
    A1腺苷受体的变构调节剂

    公开(公告)号：US07855209B2

    公开(公告)日：2010-12-21

    申请号：US11938465

    申请日：2007-11-12

    申请人： Pier Giovanni Baraldi ,  Allan R. Moorman ,  Romeo Romagnoli

    发明人： Pier Giovanni Baraldi ,  Allan R. Moorman ,  Romeo Romagnoli

    IPC分类号： A61K31/497 ,  C07D403/06

    CPC分类号： C07D333/36 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D487/08 ,  C07D487/10 ,  C07D491/10

    摘要： The present invention provides compounds of formula (I) wherein R1, R2, R3, R4 and Q have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric modulators of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain; cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke; neurological disease or injury; sleep disorder; epilepsy; and depression.

    摘要翻译： 本发明提供式（I）化合物，其中R 1，R 2，R 3，R 4和Q具有本说明书中定义的含义。 式（I）化合物是A1腺苷受体的变构调节剂，因此可用于治疗由A1腺苷受体介导的病症。 因此，式（I）化合物可用于治疗疼痛，特别是慢性疼痛如神经性疼痛; 心脏疾病或障碍，例如心脏性心律失常，例如过氧化物室上性心动过速，心绞痛，心肌梗死和中风; 神经系统疾病或损伤; 睡眠障碍; 癫痫; 和抑郁症。

    ALLOSTERIC MODULATORS OF THE A1 ADENOSINE RECEPTOR
    2.
    发明申请
    ALLOSTERIC MODULATORS OF THE A1 ADENOSINE RECEPTOR 失效
    A1腺苷受体的免疫调节剂

    公开(公告)号：US20080125438A1

    公开(公告)日：2008-05-29

    申请号：US11938465

    申请日：2007-11-12

    申请人： Pier Giovanni Baraldi ,  Allan R. Moorman ,  Romeo Romagnoli

    发明人： Pier Giovanni Baraldi ,  Allan R. Moorman ,  Romeo Romagnoli

    IPC分类号： A61K31/497 ,  C07D333/36 ,  A61P9/00 ,  A61K31/38 ,  C07D405/02

    CPC分类号： C07D333/36 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D487/08 ,  C07D487/10 ,  C07D491/10

    摘要： The present invention provides compounds of formula (I) wherein R1, R2, R3, R4 and Q have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric modulators of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain; cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke; neurological disease or injury; sleep disorder; epilepsy; and depression.

    摘要翻译： 本发明提供式（I）化合物，其中R 1，R 2，R 3，R 4， 和Q具有本说明书中定义的含义。 式（I）化合物是A 1 N 2腺苷受体的变构调节剂，因此可用于治疗由Aβ1腺苷受体介导的病症。 因此，式（I）化合物可用于治疗疼痛，特别是慢性疼痛如神经性疼痛; 心脏疾病或障碍，例如心脏性心律失常，例如过氧化物室上性心动过速，心绞痛，心肌梗死和中风; 神经系统疾病或损伤; 睡眠障碍; 癫痫; 和抑郁症。

    Adenosine A3 receptor modulators
    3.
    发明授权
    Adenosine A3 receptor modulators 有权
    腺苷A3受体调节剂

    公开(公告)号：US07271171B2

    公开(公告)日：2007-09-18

    申请号：US11169311

    申请日：2005-06-27

    申请人： Pier Giovanni Baraldi ,  Pier Andrea Borea

    发明人： Pier Giovanni Baraldi ,  Pier Andrea Borea

    IPC分类号： A01N43/54 ,  A61K31/505 ,  C07D239/00 ,  C07D471/00 ,  C07D457/00 ,  C07D491/00

    CPC分类号： A61K49/0052 ,  A61K31/519 ,  A61K49/0021 ,  A61K51/0459 ,  A61K51/0491 ,  C07B2200/05 ,  C07D471/14 ,  C07D487/14 ,  G01N33/57492 ,  G01N2333/726 ,  G01N2500/00

    摘要： The compounds of the following formula: wherein R, R2, R3 and A have the meanings given in the specification, are endowed with selective A3 adenosine receptor antagonist activity. These compounds can be used in a pharmaceutical composition to treat disorders caused by excessive activation of the A3 receptor, or can be used in a diagnostic application to determine the relative binding of other compounds to the A3 receptor. The compounds can be labeled, for example with fluorescent or radiolabels, and the labels used in vivo or in vitro to determine the presence of tumor cells which possess a high concentration of adenosine A3 receptors.

    摘要翻译： 下式的化合物：其中R，R 2，R 3和A具有说明书中给出的含义，赋予选择性A 3， 腺苷受体拮抗剂活性。 这些化合物可用于药物组合物中以治疗由过度活化的Aβ受体引起的疾病，或可用于诊断应用以确定其它化合物与A 3受体。 化合物可以被标记，例如用荧光或放射性标记，以及在体内或体外用于确定具有高浓度腺苷A 3受体的肿瘤细胞的存在的标记。

    Allosteric Enhancers of th A1 Adenosine Receptor
    7.
    发明申请
    Allosteric Enhancers of th A1 Adenosine Receptor 审中-公开
    A1腺苷受体的变构增强子

    公开(公告)号：US20120108636A1

    公开(公告)日：2012-05-03

    申请号：US13347999

    申请日：2012-01-11

    申请人： Pier Giovanni Baraldi ,  Allan R. Moorman ,  Romeo Romagnoli

    发明人： Pier Giovanni Baraldi ,  Allan R. Moorman ,  Romeo Romagnoli

    IPC分类号： A61K31/4436 ,  C07D409/04 ,  A61K31/381 ,  A61P29/00 ,  A61P9/10 ,  A61P25/08 ,  A61P25/24 ,  A61P9/00 ,  A61P9/06 ,  C07D333/36 ,  A61P25/00

    CPC分类号： C07D333/36 ,  C07D409/04

    摘要： The present invention provides compounds of formula (I) wherein W, R1, R5 and R6 have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric enhancers of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain, and inflammatory pain, cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke, neurological disease or injury, sleep disorders, epilepsy and depression.

    摘要翻译： 本发明提供式（I）化合物，其中W，R 1，R 5和R 6具有本说明书中定义的含义。 式（I）化合物是A1腺苷受体的变构增强子，因此可用于治疗由A1腺苷受体介导的病症。 因此，式（I）化合物可用于治疗疼痛，特别是慢性疼痛如神经性疼痛，炎症性疼痛，心脏病或病症如心脏性心律失常，例如过氧化物室上性心动过速，心绞痛，心肌梗死 和中风，神经系统疾病或损伤，睡眠障碍，癫痫和抑郁症。